Modulation of oestrogen receptor activity by oestrogens and anti-oestrogens.
The oestrogen receptor is a member of a supergene family that includes receptors for steroid and thyroid hormones, vitamin D3, and retinoic acid. A number of additional members of the family have been cloned where the putative ligand remains to be identified. The oestrogen receptor is a ligand-activated transcription factor that modulates specific gene expression by binding to short DNA sequences (oestrogen response elements) located in the vicinity of oestrogen-regulated genes. Regions of the receptor responsible for hormone-binding. DNA-binding and activation of transcription, have been identified. The anti-oestrogen, tamoxifen (Nolvadex), behaves as a weak oestrogen agonist. A model, based upon our current understanding of the molecular mechanism of oestrogen action, will be presented to explain the cell and gene specific effects of some anti-oestrogens.
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Imperial Chemical Industries, Central Toxicology Laboratory, Macclesfield, Cheshire, England.
D000595:Amino Acid Sequence; D004247:DNA / Q000378:metabolism; D004965:Estrogen Antagonists / Q000494:pharmacology*; D004967:Estrogens / Q000494:pharmacology*; D006801:Humans; D008954:Models, Biological; D011960:Receptors, Estrogen / Q000187:drug effects* / Q000235:genetics; D015533:Transcriptional Activation
D004965:Estrogen Antagonists; D004967:Estrogens; D011960:Receptors, Estrogen; D004247:DNA